| Description | TDO-IN-1 is an orally active, potent, and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), which inhibits indoleamine-2,3-dioxygenase.TDO-IN-1 has antitumor activity and is able to act by reversing local immune tolerance in tumor tissues. |
| In vitro | TDO-IN-1 (HT-28) 在不同肿瘤细胞线上展示了显著的杀瘤效应，处理浓度范围为0至100μM，持续时间为24小时。其对各种肿瘤细胞线的IC50值分别为：HepG2的0.54μM、Hepa1-6的5.08μM、H22的1.34μM、B16的37.39μM、MOLM-13的3.43μM以及Jurkat的7.25μM[1]。此外，在低于10μM浓度时，TDO-IN-1（0-100μM；24小时）对正常细胞（HEK 293细胞）几乎不表现出细胞毒性活性[1]。 |
| In vivo | 通过口服方式，每日一次，连续9天以25mg/kg剂量给药，TDO-IN-1 (HT-28) 能够提高表达TDO的CT26肿瘤免疫治疗的有效性。该治疗明显抑制了小鼠体内CT26肿瘤的增殖[1]。 |
| Target activity | HepG2 cells:0.54 μM, H22:1.34 μM, B16:37.39 μM, MOLM-13:3.43 μM, Jurkat cells:7.25 μM, TDO:0.62 μM, Hepa1-6:5.08 μM |
| molecular weight | 350.3 |
| Molecular formula | C16H13F3N4O2 |
| CAS | 2490672-92-7 |
| Storage | store at low temperature|Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (171.28 mM), Sonication is recommended. |
| References | 1. Huo C, et al. 4,6-Disubstituted-1H-Indazole-4-Amine derivatives with immune-chemotherapy effect and in vivo antitumor activity. Eur J Med Chem. 2022 Nov 5;241:114625. |